Heteroaryl-fused macrocyclic 2,4-diaminopyrimidine compounds of formula (I)
wherein W, G
1
, G
2
, A
1
and R
1
are defined in the description, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.
As part of our studies on pyrimidine derivatives, 27 4-alkyl-2-(1-piperazinyl)-5, 6-polymethylenepyrimidines and structurally related derivatives were synthesized, and their hypoglycemic activities were examined in mice treated with 2-deoxy-D-glucose. Most of the derivatives showed higher activity at a dose of 30 mg/kg p.o. than tolbutamide at a dose of 100 mg/kg p.o. The structure-activity relationships are discussed.